首页> 外国专利> Compounds of 7 - (benzo (b) thiophene, Furan and indolpiridil or tetrahidropiridilo), effective on systems related to serotonin.Composicionesfarmaceuticas made with such Compounds; Compounds, Intermediates useful for preparing such compounds thiophene, Furan and indolpiridilo otetr

Compounds of 7 - (benzo (b) thiophene, Furan and indolpiridil or tetrahidropiridilo), effective on systems related to serotonin.Composicionesfarmaceuticas made with such Compounds; Compounds, Intermediates useful for preparing such compounds thiophene, Furan and indolpiridilo otetr

机译:7-(苯并(b)噻吩,呋喃和吲哚哌地尔或四氢吡啶并二唑)的化合物,对与5-羟色胺有关的系统有效。化合物,可用于制备此类化合物的中间体噻吩,呋喃和吲哚哌利定

摘要

These compounds of formula I are useful to inhibit the uptake of serotonin, antagonize the 5-ht1a receptor and antagonize the 5-ht2a receptor.Through the management of people Refer to such treatment, characterized porquecantidade s effective of a compound of formula I in which X I, S, NR, S (= o) or s (= o) 2; and - C (= o) -,CH (OH) -, - C (= CH2, NOR), chnr7r, S, so or SO2; = represents a simple link or double; n is 1, 2, 3 or 4; R is H oalquilo C1 - 6; each A1A, r1b, r1c and R 2 is Regardless, h, F, CL, BR, I,Oh, alkyl C1 C1 - 6, 6 - alkoxy alkyl, Halo Alquiltio C1 C1 - 6, 6 -, phenyl -, NO2, nr7r8, - C (= o) - nr78r8, R8, nr7c (= o)CN or phenyl substituted with 1 to 3 substituents selected from the group composed of F, CL, b r, I, Oh, alquiloc1 C1 - 6, 6 - alkoxy alkyl, Halo Alquiltio C1 C1 - 6, 6 -, phenyl, NO2 or CN, NH2; R3 is H,Oh, alkyl hydroxy - C1 - 6, 6 - alkoxy alkyl C1, C1 and C1 - 6 - 6 Alquiltio; R4 esarilo, Heterocyclic cycloalkyl, aryl substituted C3 - 8 s 1 A3 Substituent selected from the group consisting of F,CL, BR, I, Oh, alkyl alkoxy C1 C1 - 6, - 6, - 6 Alquiltio haloalquilo C1, C1 - 6, phenyl, or cn or NO2, NH2; heterocycle substituted with 1 to 3 substituents selected from the grupocompuestopor F, CL, BR,I, Oh, alkyl C1 C1 - 6, 6 - alkoxy alkyl, Halo Alquiltio C1 C1 - 6, 6 -, phenyl, NO2 or CN, NH2; R5 is aryl, Heterocyclic cycloalkyl, c3-6,Arilosustituido with 1 to 3 substituents selected from the group consisting of F, CL, BR, I, Oh, I lcoxi C1 C1 - 6, - 6, 6 - hydroxy alkyl C1, C1 - 6 Halo alkyl, phenyl, NO2,NH2 or ns; or heterocycle substituted with 1 to 3 substituents selected from the group consisting of F, CL, BR, I, o, alquiloc1 - 6, 6 - alkoxy C1, C1 - 6 Hydroxy alkyl, phenyl, Alquiltio C1 - 6NO2 or CN; each of r6a and R6B is independently H or alkyl c1-3; each of R7 and R8 is H, alkyl Regardless, C1 - 6Aryl or aryl substituted with 1 to 3 substituents selected between group consisting of F, CL, BR, I, o, c1-c6 alkyl, alkoxy alkyl C1 - Halo - C1 - 6, 6, 6 Alquiltio C1 -, phenyl, NO2,NH2 or CN; and Pharmaceutical salts thereof. Are also proposed
机译:这些式I的化合物可用于抑制5-羟色胺的摄取,拮抗5-ht1a受体并拮抗5-ht2a受体。通过人的管理,参照这样的治疗方法,其特征在于porquecantidade对式I化合物有效。 XI,S,NR,S(= o)或s(= o)2;和-C(= o)-,CH(OH)-,-C(= CH2,NOR),chnr7r,S,so或SO2; =表示简单链接或双精度型; n为1、2、3或4; R是HOALQUILO C1-6; A1A,r1b,r1c和R 2各自无关,h,F,CL,BR,I,Oh,烷基C1-6-6-烷氧基烷基,卤代Alquiltio C1-1-6、6-,苯基-,NO2, nr7r8,-C(= o)-nr78r8,R8,nr7c(= o)CN或被1-3个选自F,CL,br,I,Oh,alquiloc1 C1-6、6-的取代基取代的苯基烷氧基烷基,卤代烷烃C 1 -C 6-6,苯基,NO 2或CN,NH 2; R3为H,Oh,烷基羟基-C1-6、6-烷氧基烷基C1,C1和C1-6-6Al基。 R4 esarilo,杂环环烷基,被芳基取代的C3-8 s 1 A3取代基,选自F,CL,BR,I,Oh,烷基烷氧基C1 C1-6-6-6 Alquiltio haloalquilo C1,C1-6 ,苯基或cn或NO2,NH2;被1至3个取代基取代的杂环基,所述取代基选自grupocompuestopor F,CL,BR,I,Oh,烷基C1C1-6、6-烷氧基烷基,卤代烷烃C1C1-6、6-6-,苯基,NO2或CN,NH2; R 5是芳基,杂环环烷基,c 3-6,具有1至3个选自F,CL,BR,I,Oh,I的有机取代基C 1-6,-6、6、6-羟基烷基C1,C1的取代基-6个卤代烷基,苯基,NO2,NH2或ns;或被1-3个取代基取代的杂环,所述取代基选自F,CL,BR,I,o,alquiloc1-6、6-烷氧基C1,C1-6羟基烷基,苯基,Al基C1-6NO2或CN; r6a和R6B各自独立地为H或烷基c1-3; R7和R8各自为H,烷基,无论如何,C1-6芳基或被1-3个取代基取代的芳基,所述取代基选自F,CL,BR,I,o,c1-c6烷基,烷氧基烷基C1-卤代-C1- 6,6,6 Alquiltio C1-,苯基,NO2,NH2或CN;及其药用盐。还建议

著录项

  • 公开/公告号AR019178A1

    专利类型

  • 公开/公告日2001-12-26

    原文格式PDF

  • 申请/专利权人 ELI LILLY AND COMPANY;

    申请/专利号AR1999P103129

  • 发明设计人

    申请日1999-06-29

  • 分类号C07D409/14;C07D405/14;C07D405/04;C07D409/04;C07D401/04;A61K31/4427;A61K31/4523;A61P1/00;A61P41/00;

  • 国家 AR

  • 入库时间 2022-08-22 00:46:30

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